THE PHARMACOKINETICS OF INTRAVENOUS TESTOSTERONE IN ELDERLY MEN WITH CORONARY-ARTERY DISEASE

Intracoronary testosterone injections have recently been shown to poss ess coronary vasodilating effects. The same may be true for intravenou s testosterone, but the pharmacokinetic and hemodynamic aspects need e xploration before pharmacologic studies can begin. This trial determin ed the pharmacokinetic and hemodynamic properties of 300 mu g of testo sterone given intravenously. Degree of testosterone aromatization to 1 7-beta estradiol after exogenous administration and overall patient to lerability also were evaluated. Eleven elderly men with coronary arter y disease participated in the study and were given 300 mu g of testost erone intravenously over 10 minutes. Serum blood concentrations of tes tosterone and 17-beta estradiol were measured at baseline and then per iodically Testosterone serum concentrations were stripped and fit to a two-compartment model for all patients. The volume of distribution (V darea) was 80.36 +/- 24.51 L, and the elimination half-life was 55.93 +/- 23.06 minutes. No hemodynamic differences or side effects were not ed. The serum concentrations of 17-beta estradiol were significantly i ncreased from baseline beginning 5 minutes after infusion to the end o f the study (180 minutes after infusion). Journal of Clinical Pharmaco logy, 1998;38:792-797 (C) 1998 The American College of Clinical Pharma cology.